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Search Results for " hydroxylation "

24

抑制剂 & 化合物

14

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7692	2,4-DPD	HIF	Angiogenesis; Chromatin/Epigenetic
	2,4-DPD 是氧感应酶 HIF-α 脯氨酰羟化酶 (HIF-PH) 的竞争性抑制剂。
T11847L	Liarozole R75251 dihydrochloride,利阿唑	P450; Retinoid Receptor	Metabolism
	Liarozole (R75251 dihydrochloride) 是一种咪唑衍生物，是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA)，具有抗肿瘤作用。它能够抑制维甲酸依赖的细胞色素P450(CYP26) 4- 羟基化 (IC50=7 μM)，导致组织维甲酸水平增加。
T21653	1,4-DPCA	HIF/HIF Prolyl-Hydroxylase	Chromatin/Epigenetic; Metabolism
	1,4-DPCA 是一种脯氨酰羟化酶抑制剂，对人源包皮成纤维细胞中胶原羟基化的 IC50 为 2.4 μM，对因子抑制 HIF (FIH) 的 IC50 为 60 μM。
T9624	iron chloride hexahydrate
	iron chloride hexahydrate 促进了苯基酮衍生物的选择性羟基化和氯化反应，用于构建杂四元骨架。
TQ0121	VH-298	Others; HIF; Ligand for E3 Ligase	Angiogenesis; Chromatin/Epigenetic; Others; PROTAC
	VH-298 是一种高效的 VHL:HIF-α 相互作用抑制剂(Kd:80-90 nM)。它可用于PROTAC 技术中。
T1055	Ifosfamide NSC109724,Isophosphamide,异环磷酰胺	DNA Alkylator/Crosslinker; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Ifosfamide (NSC-109724) 是一种烷化剂，具有抗肿瘤活性。它烷基化并形成 DNA 交联，从而防止 DNA 链分离和 DNA 复制。它是一种前药，必须通过肝微粒体酶的羟基化来激活。
T11277	FG 7142 ZK 39106,LSU-65	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	FG 7142 (LSU-65) 是一种非选择性苯二氮卓类反向激动剂，对含 α1 亚基的 GABAA 受体具有高亲和力，Ki 为 91 nM。它还调节 GABA 诱导的 GABAA 受体上的氯离子通量，表达 α1 亚基，EC50为 137 nM。它可增加酪氨酸羟基化并导致小鼠大脑皮层中 β-肾上腺素受体的上调。
T32743	Licodione
	Licodione is a Cytochrome P450 Monooxygenase Catalyzing 2-Hydroxylation of 5-Deoxyflavanone.
T19773	Diethyl bipy55'DC
	Diethyl bipy55'DC inhibits CP4H activity in cultured cells. The stability of collagen relies on post-translational modifications, the most prevalent being the hydroxylation of collagen strands by collagen prolyl 4-hydroxylases.
T33370	Metyrapol SU 5236,SU-5236,SU5236
	Metyrapol is a competitive inhibitor of 11-deoxycorticosterone hydroxylation by 11β-hydroxylase.
T83919	Hydroxy Darunavir R-426857
	Hydroxy darunavir是HIV-1蛋白酶抑制剂darunavir的一种代谢产物，通过异丁基脂肪族羟基化作用从darunavir形成。
T19610	(24S)-24,25-Dihydroxyvitamin D3 (24S)-24,25-Dihydroxycholecalciferol	Others	Others
	(24S)-24,25-Dihydroxyvitamin D3 undergoes various levels of hydroxylation to form active vitamin D3 analogs.
T83243	7'-Hydroxy ABA 7'-OH ABA
	7'-Hydroxy ABA (7'-OH ABA) 是由 Abscisic acid (Abscisic acid) 通过羟基化其7'-碳原子形成的代谢产物，具备显著的激素活性。
T36237	5-hydroxy Propranolol
	5-hydroxy Propranolol is a metabolite of propranolol , a β-adrenergic receptor antagonist. Propranolol is primarily metabolized in the liver, with cytochrome P450 isoform 2D6 directing ring hydroxylation and the generation of 5-hydroxy propranolol and related metabolites.
T36920	16α-hydroxy Dehydroepiandrosterone
	16α-hydroxy Dehydroepiandrosterone is a metabolite of the endogenous steroid hormone dehydroepiandrosterone .116α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosteronevia16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol .2 1.Miller, K.K.M., Cai, J., Ripp, S.L., et al.Stereo- and regioselectivity account for the diversity of dehydro...
T10661	Calcifediol-D6 骨化二醇 D6	Others	Others
	Calcifediol-D6 is the deuterated form of Calcifediol, which is a prehormone that is produced in the liver by hydroxylation of vitamin D3 by the enzyme cholecalciferol 25-hydroxylase.
T36840	(R)-Omeprazole (sodium salt)
	(R)-Omeprazole is the inactive isomer of omeprazole , a gastric proton-pump inhibitor. A stereoselective hydroxylation of (R)-omeprazole is mediated primarily by cytochrome P450 (CYP) 2C19, whereas CYP3A4 favors sulfoxidation of the active (S)-enantiomer . (R)-Omeprazole has been shown to act as a reversible direct-acting and metabolism-dependent inhibitor of CYP2C19 in pooled human liver microsomes (IC50 = 8.1 μM).
T35681	MeIQx
	MeIQx (MeIQx) is a food-derived carcinogen that has been found in high temperature-cooked fish and meats.1It is activated by hydroxylation and subsequent O-acetylationviathe cytochrome P450 (CYP) isoform CYP1A2 and N-acetyltransferase 2, respectively, in UV5 cells expressing the human enzymes to a metabolite that reacts with DNA to form adducts.2MeIQx (200 and 400 ppm in the diet) induces tumor formation in rats.3
T35708	N-acetyl-5-Aminosalicylic Acid
	N-acetyl-5-Aminosalicylic acid is a metabolite of the anti-inflammatory agent 5-aminosalicylic acid and its prodrug form, sulfasalazine . It is formed in the liver, intestinal lumen, and colonic epithelial cells via N-acetyltransferases. It reduces IFN-γ binding to colonic epithelial cells by 24% when used at a concentration of 10 mM. N-acetyl-5-Aminosalicylic acid (100 μM) scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay and inhibits base hydroxylation in DNA stimulated by ...
T75141	Aflatoxin Q1
	Aflatoxin Q1是Aflatoxin B1 (AFB1)的羟基化代谢产物，后者由黄曲霉 (A. flavus) 产生的一种霉菌毒素。在人肝微粒体中，不论底物浓度高低，Aflatoxin B1的8,9-氧化物及Aflatoxin Q1均为其主要氧化产物。将Aflatoxin B1 3α-羟基化生成Aflatoxin Q1被视为一条重要的解毒途径。
T36384	DL-Tyrosine-13C9,15N L-Tyrosine-13C9,15N
	L-Tyrosine-13C9,15N is intended for use as an internal standard for the quantification of L-tyrosine by GC- or LC-MS. L-Tyrosine is a non-essential amino acid.1It is produced by hydroxylation of phenylalanine by phenylalanine hydroxylase but can also be obtained from dietary sources or degradation of endogenous proteins, resulting in L-tyrosine release.1,2L-Tyrosine is a precursor in the biosynthesis of catecholamine neurotransmitters, melanins, and thyroid hormones.3Plasma, skeletal muscle, and...
T37361	6β-hydroxy Dexamethasone
	6β-hydroxy Dexamethasone is a metabolite of dexamethasone that is more hydrophilic than the parent compound. Dexamethasone is metabolized by CYP3A4; therefore, quantification of the dexamethasone metabolites, 6α- and 6β-hydroxy dexamethasone, can be used to determine CYP3A4 enzyme activity in humans., The formation of 6-hydroxy dexamethasone metabolites is species-specific, with hamsters producing the highest amount. In rats, dexamethasone hydroxylation is sex-specific, with male rats producing ...
T78135	Nicotelline Nicotellin
	Nicotelline（Nicotellin）是一种与尼古丁相关的生物碱，作为人类cDNA表达的细胞色素P-450 2A6（CYP2A6）的弱抑制剂，不显著抑制该酶介导的香豆素7-羟基化反应，在300 μM浓度下效果更是如此。此外，Nicotelline还被用作烟草烟雾中颗粒物（PM）的示踪剂和生物标记物。
T79343	hCYP3A4-IN-1
	hCYP3A4-IN-1（化合物C6）是一种经口服时具有活性的hCYP3A4抑制剂，其对hCYP3A4的IC50值在人肝微粒体(HLM)为43.93 nM，在CHO-3A4稳定转染细胞系中为153.00 nM。hCYP3A4-IN-1通过竞争性抑制机制，有效抑制CYP3A4催化的N-乙基-1,8-萘二甲酰亚胺(NEN)羟基化反应，其Ki值为30.00 nM。

化合物

Cat.No: T7692

Target: HIF

Cat.No: T11847L

Synonym: R75251 dihydrochloride,利阿唑

Target: P450, Retinoid Receptor

Cat.No: T21653

Target: HIF/HIF Prolyl-Hydroxylase

iron chloride hexahydrate

Cat.No: T9624

Cat.No: TQ0121

Target: Others, HIF, Ligand for E3 Ligase

Cat.No: T1055

Synonym: NSC109724,Isophosphamide,异环磷酰胺

Target: DNA Alkylator/Crosslinker, DNA/RNA Synthesis

Cat.No: T11277

Synonym: ZK 39106,LSU-65

Target: GABA Receptor

Cat.No: T32743

Diethyl bipy55'DC

Cat.No: T19773

Cat.No: T33370

Synonym: SU 5236,SU-5236,SU5236

Hydroxy Darunavir

Cat.No: T83919

Synonym: R-426857

(24S)-24,25-Dihydroxyvitamin D3

Cat.No: T19610

Synonym: (24S)-24,25-Dihydroxycholecalciferol

Target: Others

Cat.No: T83243

Synonym: 7'-OH ABA

5-hydroxy Propranolol

Cat.No: T36237

16α-hydroxy Dehydroepiandrosterone

Cat.No: T36920

Cat.No: T10661

Synonym: 骨化二醇 D6

Target: Others

(R)-Omeprazole (sodium salt)

Cat.No: T36840

Cat.No: T35681

N-acetyl-5-Aminosalicylic Acid

Cat.No: T35708

Cat.No: T75141

DL-Tyrosine-13C9,15N

Cat.No: T36384

Synonym: L-Tyrosine-13C9,15N

6β-hydroxy Dexamethasone

Cat.No: T37361

Cat.No: T78135

Synonym: Nicotellin

Cat.No: T79343

Cat. No.	Product Name	Target	Signaling Pathways
T3S0804	Worenine 甲基黄连碱,Worenin	Others	Others
	Worenine (Worenin) 是一种从黄连中提取的物质。它在大鼠体内第一阶段代谢中显示出脱氢，氢化，羟基化和脱亚甲基反应。在大鼠体内 II 期代谢中显示为硫酸化和葡萄糖醛酸化反应。
T3696	polygalaxanthone III	Others; P450	Metabolism; Others
	Polygalaxanthone III 提取自远志polygala tenuifolia wild，可抑制CYP450酶。它能够抑制由 CYP2E1 催化的氯唑沙宗 6-羟基化(IC50:50.56μM)。
T3397	Epmedin C 淫羊霍定C,Baohuoside-VI,Epimedin C	Others	Others
	Epmedin C (Baohuoside-VI) 是天然化合物，在切除卵巢的小鼠体内与雌性激素作用相似。
T3881	Vaccarin	Integrin; Akt; PERK; AMPK	Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	Vaccarin 是从王不留行中提取的一种黄酮糖苷，可显著促进伤口愈合以及伤口部位的内皮和成纤维细胞增殖。它通过激活 AMPK 信号通路改善胰岛素抵抗和脂肪变性。
T2S2211	Tenuifoliside C	Dehydrogenase	Metabolism
	Tenuifoliside C 是从野生的 polygala tenuifolia 中分离得到的。它对 CYP2E1 催化氯唑酮 6-羟基化反应具有抑制作用。
T4A2458	Resibufogenin 酯蟾毒配基,Bufogenin,Recibufogenin,酯蟾毒配基，蟾力苏	Others	Others
	Resibufogenin (Bufogenin) 是华蟾素的成分之一，表现出抑制氧化应激及肿瘤再生的活性。
T3818	Fraxinol	Others; P450	Metabolism; Others
	Fraxinol 是一种分离自半边莲中的化合物。
T19394	L-hydroxylysine dihydrochloride (2S,5R)-5-Hydroxylysine dihydrochloride	Others	Others
	L-hydroxylysine dihydrochloride , is formed by posttranslational hydroxylation of some lysine residues. It is an amino acid, is exclusive to collagen protein.
T83241	7-Hydroxy-TSU-68
	7-Hydroxy-TSU-68为TSU-68的衍生物，该化合物为TSU-68在人类肝微粒体内经生物转化途径形成的代谢产物，其含量标识了TSU-68自身诱导的羟基化程度。
TN2144	Resveratroloside	P450; NO Synthase	Immunology/Inflammation; Metabolism
	Resveratroloside 是α-glucosidase 的竞争性抑制剂，可以对血糖水平进行调节，对心脏具有保护作用。
TMA2106	(-)-Sparteine	P450	Metabolism
	Sparteine is a class 1a antiarrhythmic agent, a sodium channel blocker. The deficient debrisoquine hydroxylation of Sparteine is due to the absence of P-450IID1 protein in the livers of poor metabolizers.
T38557	Chitotriose trihydrochloride
	Chitotriose trihydrochloride is an orally active chitooligosaccharide known for its antioxidant properties. It effectively inhibits the hydroxylation of benzoate to salicylate by H 2 O 2 in the presence of Cu 2+, with an IC 50 value of 80 μM.
T36915	21-Deoxycortisol
	21-Deoxycortisol is a corticosteroid metabolite of 17-hydroxyprogesterone produced in the adrenal glandvia11-hydroxylation by 11β-hydroxylase.1,2Serum levels of 21-deoxycortisol are elevated in patients with congenital adrenal hyperplasia that are heterozygous for mutations inCYP2A21, the gene encoding steroid 21-hydroxylase, and have been used as a biomarker for the detection of 21-hydroxylase deficiencies. 1.Fiet, J., Villette, J.-M., Galons, H., et al.The application of a new highly-sensitive...
T83264	6-Hydroxy-TSU-68
	6-Hydroxy-TSU-68为TSU-68的衍生物，此化合物为TSU-68在人肝微粒体生物转化路径中的代谢产物，其含量反映TSU-68的自诱导羟基化程度。

天然产物

Cat.No: T3S0804

Synonym: 甲基黄连碱,Worenin

Target: Others

polygalaxanthone III

Cat.No: T3696

Target: Others, P450

Cat.No: T3397

Synonym: 淫羊霍定C,Baohuoside-VI,Epimedin C

Target: Others

Cat.No: T3881

Target: Integrin, Akt, PERK, AMPK

Tenuifoliside C

Cat.No: T2S2211

Target: Dehydrogenase

Cat.No: T4A2458

Synonym: 酯蟾毒配基,Bufogenin,Recibufogenin,酯蟾毒配基，蟾力苏

Target: Others

Cat.No: T3818

Target: Others, P450

L-hydroxylysine dihydrochloride

Cat.No: T19394

Synonym: (2S,5R)-5-Hydroxylysine dihydrochloride

Target: Others

7-Hydroxy-TSU-68

Cat.No: T83241

Resveratroloside

Cat.No: TN2144

Target: P450, NO Synthase

Cat.No: TMA2106

Target: P450

Chitotriose trihydrochloride

Cat.No: T38557

21-Deoxycortisol

Cat.No: T36915

6-Hydroxy-TSU-68

Cat.No: T83264

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